Lamivudine is a nucleoside reverse transcriptase inhibitor, and is a kind of deoxycytidine analogue, which can inhibit the reproduction of Human immunodeficiency virus (HIV) and hepatitis B virus (HBV), whose chemical name is (2R-cis)-4-amino-1-(2-hydroxymethyl-1,3-oxathiolan-5-yl)-1H-pyrimidin-2-one, and structural formula is as follows:

In 1990, Belleau et al firstly reported Lamivudine structure, and BioChem Pharma of Canada firstly developed Lamivudine to be used to treat AIDS (WO91/17159) and hepatitis B (EP0474119), and found that it had distinguished therapeutic effect on hepatitis B. Since Lamivudine has two chiral centers, it has 4 stereisomers, among which the 2R,5S (2R-cis)-isomer is the most potent in anti-HIV and anti-HBV activities, and its cytotoxicity on some cells is lower than its enantiomer or racemic body.
WO94/14802 mentioned two synthetic schemes (see Scheme 1 and Scheme 2):


In the above two schemes of this process, chirality was not controlled, and the final product was obtained by column chromatography, thus the yield was low and the requirement on the equipment was high, resulting in that the production cost was high and the operation in the production could not be controlled easily.